2,4‐Disubstituted Pyrimidines: A Novel Class of KDR Kinase Inhibitors.

Abstract 2,4-Disubstituted pyrimidines were synthesized as a novel class of KDR kinase inhibitors. Evaluation of the SAR of the screening lead compound 1 (KDR IC 50 =105 nM, Cell IC 50 =8% inhibition at 500 nM) led to the potent 3,5-dimethylaniline derivative 2d (KDR IC 50 =6 nM, cell IC 50 =19 nM).